公开(公告)号：US11759464B2

公开(公告)日：2023-09-19

申请号：US16619702

申请日：2018-06-05

申请人： ObsEva S.A.

发明人： Ernest Loumaye ,  Jean-Pierre Gotteland ,  Oliver Pohl

IPC分类号： A61K31/519 ,  A61K31/565 ,  A61P5/00 ,  A61K31/57

CPC分类号： A61K31/519 ,  A61K31/565 ,  A61K31/57 ,  A61P5/00

摘要： The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.

公开(公告)号：US20200179390A1

公开(公告)日：2020-06-11

申请号：US16619702

申请日：2018-06-05

申请人： OBSEVA S.A.

发明人： Ernest LOUMAYE ,  Jean-Pierre GOTTELAND ,  Oliver POHL

IPC分类号： A61K31/519 ,  A61K31/57 ,  A61K31/565 ,  A61P5/00

摘要： The invention provides compositions and methods for reducing the volume of menstrual blood loss in a patient, such as a human patient, for instance, that has uterine fibroids, by administration of a gonadotropin-releasing hormone (GnRH) antagonist. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxypheny I]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof.

公开(公告)号：US20200155515A1

公开(公告)日：2020-05-21

申请号：US16752961

申请日：2020-01-27

申请人： ObsEva S.A.

发明人： Patrick Naxos PAGE ,  Matthias SCHWARZ ,  Catherine JORAND-LEBRUN ,  Anna QUATTROPANI ,  Vincent POMEL ,  Ernest LOUMAYE ,  Oliver POHL ,  Jean-Pierre GOTTELAND

IPC分类号： A61K31/426 ,  A61K9/00 ,  A61P15/06 ,  A61K45/06 ,  A61K31/40 ,  A61K31/4422 ,  A61K38/095

摘要： The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as preterm labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

公开(公告)号：US10478420B2

公开(公告)日：2019-11-19

申请号：US15952934

申请日：2018-04-13

申请人： ObsEva S.A.

发明人： Andre Chollet ,  Oliver Pohl

IPC分类号： A61K31/401 ,  A61K9/20 ,  A61K45/06 ,  A61K9/00 ,  A61K47/40 ,  A61K31/40 ,  A61P15/08

摘要： The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one-O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.

公开(公告)号：US20160221944A1

公开(公告)日：2016-08-04

申请号：US14917847

申请日：2014-07-25

申请人： ObsEva S.A.

发明人： Andre CHOLLET

IPC分类号： C07D207/22

摘要： The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methl9243yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.

摘要翻译： 本发明涉及式（3Z，5S）-5-（羟甲基）-1 - [（2'-甲基-1,1'-联苯-4-基）羰基]吡咯烷-3-酮O- 甲基9243肟，和/或其在催产素受体和/或加压素V1a受体上具有拮抗作用的活性代谢物，其制备方法，含有它们的药物组合物及其用途。

公开(公告)号：US20230321052A1

公开(公告)日：2023-10-12

申请号：US17984833

申请日：2022-11-10

申请人： ObsEva S.A.

发明人： Patrick Naxos PAGE ,  Matthias SCHWARZ ,  Catherine JORAND-LEBRUN ,  Anna QUATTROPANI ,  Vincent POMEL ,  Ernest LOUMAYE ,  Oliver POHL ,  Jean-Pierre GOTTELAND

IPC分类号： A61K31/426 ,  A61K9/00 ,  A61P15/06 ,  A61K45/06 ,  A61K31/40 ,  A61K31/4422 ,  A61K38/095

CPC分类号： A61K31/426 ,  A61K9/0053 ,  A61P15/06 ,  A61K45/06 ,  A61K9/0019 ,  A61K31/40 ,  A61K31/4422 ,  A61K38/095 ,  A61K9/20

摘要： The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as preterm labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

公开(公告)号：US11524003B2

公开(公告)日：2022-12-13

申请号：US16752961

申请日：2020-01-27

申请人： ObsEva S.A.

发明人： Patrick Naxos Page ,  Matthias Schwarz ,  Catherine Jorand-Lebrun ,  Anna Quattropani ,  Vincent Pomel ,  Ernest Loumaye ,  Oliver Pohl ,  Jean-Pierre Gotteland

IPC分类号： A61K31/426 ,  A61K9/00 ,  A61P15/06 ,  A61K45/06 ,  A61K31/40 ,  A61K31/4422 ,  A61K38/095 ,  A61K9/20 ,  A61K9/48 ,  A61K9/16

摘要： The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as preterm labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

公开(公告)号：US20220117969A1

公开(公告)日：2022-04-21

申请号：US17289418

申请日：2019-10-29

申请人： ObsEva S.A.

发明人： Jean-Pierre GOTTELAND ,  Ernest LOUMAYE

IPC分类号： A61K31/519 ,  A61K47/54 ,  A61K31/513 ,  A61K31/4184 ,  A61K31/4439 ,  A61K31/585 ,  A61K31/573 ,  A61K31/565 ,  A61K31/567 ,  A61K31/57 ,  A61P15/00 ,  A61K31/55

摘要： The present disclosure provides compositions and methods for treating endometrial growth disorders in a patient, such as a human patient, and particularly pre-menopausal female human patients. Exemplary disorders that may be treated using the compounds and therapeutic regimens described herein include adenomyosis and rectovaginal endometriosis. The compounds described herein that may be used to treat such indications include gonadotropin-releasing hormone (GnRH) antagonists. Suitable GnRH antagonists useful in conjunction with the compositions and methods described herein include thieno[3,4d]pyrimidine derivatives, such as 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno [3,4d]pyrimidine-5-carboxylic acid and the choline salt thereof, among others.

公开(公告)号：US20200281892A1

公开(公告)日：2020-09-10

申请号：US16569065

申请日：2019-09-12

申请人： ObsEva S.A.

发明人： Andre CHOLLET ,  Oliver POHL

IPC分类号： A61K31/40 ,  A61K31/401 ,  A61K9/20 ,  A61K9/00 ,  A61K47/40 ,  A61P15/08 ,  A61K45/06

摘要： The present invention relates to solid oral formulations comprising a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one-O-methyloxime, and/or an active metabolite thereof, and the use of said formulations in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea and embryo implantation failure due to uterine contractions. The present invention is furthermore related to processes for their preparation.

公开(公告)号：US09670155B2

公开(公告)日：2017-06-06

申请号：US14479664

申请日：2014-09-08

申请人： ObsEva S.A.

发明人： Andre Chollet

IPC分类号： C07D207/22 ,  C07D207/09

CPC分类号： C07D207/22 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/40 ,  C07D207/09

摘要： The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2′-methyl-1,1′-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methy19243-yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.